Review
Biochemistry & Molecular Biology
Mateusz Kciuk, Adrianna Gielecinska, Somdutt Mujwar, Mariusz Mojzych, Beata Marciniak, Rafal Drozda, Renata Kontek
Summary: Carbonic anhydrases IX and CAXII play crucial roles in cancer and have become a focus in anticancer drug design. This offers an opportunity to develop new targeted therapies with fewer side effects.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Toni C. Denner, Andrea Angeli, Marta Ferraroni, Claudiu T. Supuran, Rene Csuk
Summary: Sulfonamides have inhibitory effects on carbonic anhydrases, and sulfonamides with biphenyl- and benzylphenyl substitutions show high selectivity for the treatment of hypoxic cancers and potential applications in treating cerebral edema.
Article
Biochemistry & Molecular Biology
Andrea Angeli, Victor Kartsev, Anthi Petrou, Mariana Pinteala, Volodymyr Brovarets, Roman Vydzhak, Svitlana Panchishin, Athina Geronikaki, Claudiu T. Supuran
Summary: A series of novel benzenesulfonamides incorporating pyrazole- and pyridazinecarboxamides decorated with bulky moieties were synthesized and investigated for their inhibitory effects on various human carbonic anhydrase isoforms. Isoform-selective inhibitors were obtained, with a computational approach employed to explain the observed selectivity, potentially useful in drug design for developing inhibitors with pharmacological applications such as antiglaucoma, diuretic, antitumor, or anti-cerebral ischemia drugs.
Article
Chemistry, Medicinal
Baijayantimala Swain, Santosh Kumar Sahoo, Priti Singh, Andrea Angeli, Venkata Madhavi Yaddanapudi, Claudiu T. Supuran, Mohammed Arifuddin
Summary: A series of novel sulfonamide containing quinoline compounds were synthesized and tested for their inhibitory activity against human carbonic anhydrase isoforms I, II, IX and XII. Most of the compounds showed potent inhibitory activity, with some being more effective than the standard drug acetazolamide. 4-substituted benzenesulfonamides exhibited higher potency than 3-substituted derivatives.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Moataz Shaldam, Alessio Nocentini, Zainab M. Elsayed, Tamer M. Ibrahim, Rofaida Salem, Ramadan A. El-Domany, Clemente Capasso, Claudiu T. Supuran, Wagdy M. Eldehna
Summary: A new series of quinoline-based benzenesulfonamides (QBS) have been developed as potential carbonic anhydrase inhibitors, with para-sulphonamide derivatives showing the best inhibitory activity. In addition, a linker elongation approach and molecular docking simulation studies were used to further investigate the anticancer effects of QBS.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Afaf El-Malah, Ehab S. Taher, Andrea Angeli, Samar S. Elbaramawi, Zeinab Mahmoud, Nour Moustafa, Claudiu T. Supuran, Tarek S. Ibrahim
Summary: A series of novel quinoline derivatives with sulfonamide as zinc-binding group (ZBG) were synthesized as carbonic anhydrase (CA) inhibitors. The compounds exhibited efficient inhibition against tumor-associated CA isoforms IX and XII, with one particular hybrid 10b demonstrating significant activity against MCF-7 cancer cells under normal and hypoxic conditions. The compounds also induced apoptosis in MCF-7 and MDA-MB-231 cells and altered the Bax/Bcl expression ratio. Docking studies supported the biological findings, indicating the effectiveness of the regioisomeric tactic for the quinoline-based sulfonamide molecules in inhibiting tumor-relevant hCAs IX/XII.
BIOORGANIC CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Suleyman Akocak, Nebih Lolak, Simone Giovannuzzi, Claudiu T. Supuran
Summary: This research introduces a series of compounds that exhibit significant inhibitory activity against tumor-associated isoforms of carbonic anhydrase, with certain selectivity. Investigating the structure-activity relationships of these compounds could provide insights for the development of novel therapeutic agents targeting hypoxic tumors.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Biochemistry & Molecular Biology
Chnar Kakakhan, Cuneyt Turkes, Ozcan Gulec, Yeliz Demir, Mustafa Arslan, Gizem Ozkemahli, Sukru Beydemir
Summary: A series of novel inhibitors of human alpha-carbonic anhydrase (hCA) were designed using a tail approach. These inhibitors showed remarkable selectivity for tumor isoforms hCA IX and XII. Adding a lipophilic naphthyl tail to the analogues increased the inhibitory and selective activities against hCA XII. The compounds also exhibited inhibitory effects against a human lung adenocarcinoma cancer cell line.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Erden Banoglu, Taner Ercanli, Tugce Gur Maz, Daniela Vullo, Alessandro Bonardi, Paola Gratteri, Claudiu T. Supuran
Summary: A series of newly synthesized thiadiazolyl-benzenesulfonamide derivatives exhibited significant inhibitory activity against human carbonic anhydrase, with some compounds showing dual inhibition against two isoforms. The nature of substituents at the tail part of the main scaffold influenced the activity and selectivity towards different isoforms, with compound 17 demonstrating the most potent inhibitory effects.
Article
Biochemistry & Molecular Biology
Leonardo E. Riafrecha, Macarena S. Le Pors, Martin J. Lavecchia, Silvia Bua, Claudiu T. Supuran, Pedro A. Colinas
Summary: New C-glycosides and alpha,beta-unsaturated ketones containing the vanillin moiety have been studied as inhibitors of carbonic anhydrase isoforms. Some derivatives show selectivity for tumor-associated CA isoforms, indicating potential for therapeutic applications in hypoxic tumors and other pathologies.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Laura De Luca, Andrea Angeli, Federico Ricci, Claudiu T. Supuran, Rosaria Gitto
Summary: In recent years, the use of multistep hybrid computational protocols in drug discovery of enzyme inhibitors has gained attention. This study successfully generated pharmacophore models for hCA VA inhibitors using a combination of ligand- and structure-based approaches. Virtual screening on a database of commercially available sulfonamides resulted in the identification of several potential inhibitors.
ARCHIV DER PHARMAZIE
(2023)
Article
Biochemistry & Molecular Biology
Vaha Akbary Moghaddam, Vesal Kasmaeifar, Zainab Mahmoodi, Hossein Ghafouri, Omid Saberi, Asadollah Mohammadi
Summary: A novel derivative of sulfamethoxazole named ZM-093 was synthesized and characterized through experimental and computational analysis, showing significant inhibitory effect against the cancer-related protein HSP70, potentially through binding to its substrate-binding domain. Additionally, a new method for evaluating the inhibitory activity of ligands to HSP70 based on protonography was introduced.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Article
Chemistry, Medicinal
Moataz Shaldam, Wagdy M. Eldehna, Alessio Nocentini, Zainab M. Elsayed, Tamer M. Ibrahim, Rofaida Salem, Ramadan A. El-Domany, Clemente Capasso, Hatem A. Abdel-Aziz, Claudiu T. Supuran
Summary: This study describes the design of benzofuran-based derivatives as potential carbonic anhydrase inhibitors, with modifications in tail and spacer structures to enhance inhibitory activities against tumor-related CA isoforms. The synthesized compounds showed efficient inhibition of CA IX isoform and promising anticancer and pro-apoptotic activities towards cancer cell lines.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Jekaterina Ivanova, Morteza Abdoli, Alessio Nocentini, Raivis Zalubovskis, Claudiu T. Supuran
Summary: A series of 4-methyl-1,2,3-benzoxathiazine-2,2-dioxides with different substituents were synthesized. The compounds showed nanomolar inhibitory effects on target hCA IX and XII, while exhibiting low or no inhibitory properties on off-target hCA I and moderate inhibition on hCA II. The derivatives of 4-methyl-1,2,3-benzoxathiazine 2,2-dioxide demonstrated excellent selectivity towards CA IX/XII over hCA I and very good selectivity towards CA IX/XII over hCA II.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Simone Giovannuzzi, Mario D'Ambrosio, Cristina Luceri, Sameh Mohamed Osman, Marco Pallecchi, Gianluca Bartolucci, Alessio Nocentini, Claudiu T. Supuran
Summary: This article presents a new drug design strategy for producing membrane-impermeant carbonic anhydrase inhibitors that selectively target tumor-associated CAs IX and XII. The study shows that this drug design strategy can achieve selective inhibition of tumor-associated CAs.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Chemistry, Medicinal
Morteza Abdoli, Viviana De Luca, Clemente Capasso, Claudiu T. T. Supuran, Raivis Zalubovskis
Summary: Two novel sulfaguanidine series were synthesized by desulfidative amination of dimethyl arylsulfonylcarbonimidodithioates. These compounds were tested for their inhibition of human carbonic anhydrase isozymes. The N-(N-alkyl/benzyl-carbamimidoyl) benzenesulfonamide derivatives showed higher inhibitory activity than the N-(N,N'-dialkyl/dibenzyl-carbamimidoyl) benzenesulfonamide derivatives.
Article
Biochemistry & Molecular Biology
Morteza Abdoli, Viviana De Luca, Clemente Capasso, Claudiu T. T. Supuran, Raivis Zalubovskis
Summary: A library of novel thiazolone-benzenesulphonamides was synthesized and evaluated for their inhibitory activity against human cytosolic carbonic anhydrases and bacterial carbonic anhydrases. The prepared compounds 4a-4j showed low nanomolar range inhibition against all investigated hCAs. Compound 4d exhibited strong inhibition against bacterial MscCA beta with a K-I of 73.6 nM, much better than AAZ. The tested compounds showed medium inhibitory potency against StCA1 compared to the standard drug, while poorly inhibited StCA2.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Doretta Cuffaro, Riccardo Di Leo, Lidia Ciccone, Alessio Nocentini, Claudiu T. Supuran, Elisa Nuti, Armando Rossello
Summary: Carbonic anhydrases (CAs) are enzymes that catalyze the hydration of carbon dioxide, playing important roles in physiological processes. This study investigated a new series of isoxazoline-based amino alcohols as CA activators and found that compounds 3 and 5 showed the best activation effects towards hCA VII, with submicromolar affinity and good selectivity over hCA I. These newly identified CA activators have potential therapeutic applications in aging, epilepsy, and neurodegeneration.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Review
Infectious Diseases
Alessio Nocentini, Clemente Capasso, Claudiu T. Supuran
Summary: Resistance to antibiotic treatment occurs when microorganisms resist clinically approved antibiotics. Medication repurposing/repositioning is a strategy that can help find new antibiotics. Among them, Zn2+ ion binders, such as sulfonamides and their bioisosteres, are considered promising compounds for obtaining novel antibacterials.
Article
Chemistry, Multidisciplinary
Belma Zengin Kurt, Gulsen Celebi, Dilek Ozturk Civelek, Atilla Akdemir, Andrea Angeli, Fatih Sonmez, Claudiu T. Supuran
Summary: In this study, sixty novel coumarin-monoterpene compounds were synthesized and evaluated for their inhibitory effects on hCA isoforms and anticancer potentials. All synthesized molecules selectively inhibited CA IX and XII, with compounds 23 and 42 showing the strongest inhibitory activity against hCA IX. Cytotoxicity evaluation revealed that compounds 14 and 63 exhibited the highest cytotoxicity on MCF-7 cells, while compound 23 showed the strongest cytotoxic effect on both PC-3 and HT-29 cell lines. Furthermore, compounds 14, 23, and 66 showed a reduction in CA IX and CA XII protein expression and increased apoptosis in different cell lines. The modeling studies demonstrated that only the open coumarin form of the compounds could interact directly with the active-site Zn2+ ion.
Article
Oncology
Aditi Redij, Simone Carradori, Andrea Petreni, Claudiu T. Supuran, Mrunmayee P. Toraskar
Summary: This study synthesized a series of coumarin derivatives incorporating pyrazole-1-carboxamide moiety and evaluated their inhibitory activity against carbonic anhydrase. The results showed that these compounds did not inhibit the widespread CA I and II, but showed sub-micromolar inhibitory activity against CA IX and XII with high selectivity.
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
(2023)
Review
Biochemistry & Molecular Biology
Sridhar Goud Nerella, Priti Singh, Pavitra S. Thacker, Mohammed Arifuddin, Claudiu T. Supuran
Summary: Positron emission tomography (PET) and fluorescent imaging are important in medical diagnosis, oncologic research, and drug development. PET estimates physiological changes at the molecular level using radiotracers, while fluorescent imaging detects molecular level changes using labeled probes. This review focuses on PET radiotracers and fluorescent probes for diagnosing and treating tumors expressing hCA IX and hCA XII.
BIOORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Valentina Puca, Gabriele Turacchio, Beatrice Marinacci, Claudiu T. Supuran, Clemente Capasso, Pamela Di Giovanni, Ilaria D'Agostino, Simone Carradori, Rossella Grande
Summary: The World Health Organization has identified Helicobacter pylori as a high-priority pathogen requiring updated antibacterial treatments. This study investigated the potential of combining a CA inhibitor, carvacrol (CAR), amoxicillin (AMX), and a urease inhibitor (SHA) to develop a multiple-targeted anti-H. pylori therapy. The combinations of these compounds showed strong inhibition of H. pylori growth and biofilm formation, with CAR-AMX and CAR-SHA combinations demonstrating additive effects and AMX-SHA combination showing indifferent effects.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Editorial Material
Biochemistry & Molecular Biology
Claudiu T. Supuran
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Zainab M. M. Elsayed, Hadia Almahli, Alessio Nocentini, Andrea Ammara, Claudiu T. T. Supuran, Wagdy M. M. Eldehna, Sahar M. M. Abou-Seri
Summary: In this study, a new series of non-classical CA inhibitors, 2-aryl-quinazolin-4-yl aminobenzoic acid derivatives, were designed and synthesized as potential anticancer candidates. The inhibitory activities of these compounds against different CA isoforms were evaluated, and selected compounds were further tested for their anti-proliferative activity against human cancer cell lines.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Andrea Angeli, Marta Ferraroni, Alessandro Bonardi, Claudiu T. Supuran, Alessio Nocentini
Summary: Carbonic anhydrases (CAs) are important zinc metalloenzymes that catalyze the hydration of carbon dioxide. They play crucial roles in various biological processes and can be targeted for the treatment of diseases like glaucoma, obesity, and cancer. In this study, we report the co-crystallization of a N-nitro sulphonamide derivative with human CA II, revealing the binding site and mode of inhibition. This knowledge could aid in the development of more potent and selective CA inhibitors.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Morteza Abdoli, Alessandro Bonardi, Niccolo Paoletti, Ashok Aspatwar, Seppo Parkkila, Paola Gratteri, Claudiu T. Supuran, Raivis Zalubovskis
Summary: A library of structurally diverse N-((4-sulfamoylphenyl)carbamothioyl) amides was synthesized by selectively acylating 4-thioureidobenzenesulfonamide with various acyl chlorides. The inhibitory effects of these sulfonamides on human carbonic anhydrase (hCA) and bacterial beta-carbonic anhydrase from Mycobacterium tuberculosis (MtCA) were investigated in vitro and in silico. The compounds showed better inhibition against hCA I, hCA II, hCA VII, as well as MtCA1 and MtCA2, but poor inhibition against MtCA3.
Article
Chemistry, Medicinal
Ilaria D'Agostino, Susi Zara, Simone Carradori, Viviana De Luca, Clemente Capasso, Clemens H. M. Kocken, Anne-Marie Zeeman, Andrea Angeli, Fabrizio Carta, Claudiu T. Supuran
Summary: The hybrid compounds synthesized in this study, which combine the Artesunate core with a sulfonamide moiety, showed high inhibition potency against the protozoan PfCA, while exhibiting low cytotoxic effects on human cells, indicating a wide therapeutic window.
Article
Chemistry, Organic
Maria Giulia Davighi, Camilla Matassini, Andrea Goti, Marta Ferraroni, Andrea Angeli, Claudiu T. Supuran, Francesca Cardona
Summary: A series of novel mono- and three-tailed derivatives containing a sugar or an iminosugar with a terminal benzenesulfonamide were synthesized to investigate their inhibitory activity and selectivity towards human carbonic anhydrases (hCAs). Copper-catalyzed azide-alkyne cycloaddition followed by an amine-isothiocyanate coupling was used for synthesis. Biological assays revealed that the single-tailed sugar-based compound 10 exhibited better inhibition against three different hCAs compared to the reference compound (AAZ), while the three sugar tailed derivatives 25 and 26 showed potent and selective inhibition. The iminosugar single-tailed compound 31 exhibited promising and selective inhibitory activity towards hCA VII (Ki = 9.7 nM).
ORGANIC & BIOMOLECULAR CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Toni C. Denner, Andrea Angeli, Marta Ferraroni, Claudiu T. Supuran, Rene Csuk
Summary: Sulfonamides have inhibitory effects on carbonic anhydrases, and sulfonamides with biphenyl- and benzylphenyl substitutions show high selectivity for the treatment of hypoxic cancers and potential applications in treating cerebral edema.
Correction
Biochemistry & Molecular Biology
Mohamed Marzouk, Shimaa M. Khalifa, Amal H. Ahmed, Ahmed M. Metwaly, Hala Sh. Mohammed, Hanan A. A. Taie
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Gerardo Andres Libreros-Zuniga, Danilo Pava e Pavao, Vinicius de Morais Barroso, Nathalya Cristina de Moraes Roso Mesquita, Saulo Fehelberg Pinto Braga, Glaucius Oliva, Rafaela Salgado Ferreira, Kelly Ishida, Marcio Vinicius Bertacine Dias
Summary: Tuberculosis is a major global cause of death, and the emergence of drug-resistant strains has increased the burden of this disease. New alternative therapies are constantly needed, and recent research has identified small molecules as potential inhibitors of Ldts in M. tuberculosis, which have antimycobacterial activity.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Xiao-Dong Wang, Yong-Si Liu, Ming-Hao Hu
Summary: In this study, a selffolded fluorescent probe was designed to selectively illuminate G4s by unfolding its intramolecular aggregation mediated by G4 binding. This probe showed more controllable background emission and promising ability to track G4 forming dynamics compared to previous disaggregation-induced emission (DIE) probes.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yu Xiang, Zhuo Yuan, Qichuan Deng, Linshen Xie, Dongke Yu, Jianyou Shi
Summary: This review provides a brief description of the diagnosis, pathogenesis, and potential therapeutic inhibitors for renal fibrosis. Currently, there are no clear therapeutic targets or drugs for renal fibrosis; however, some natural products may have potential efficacy for treating renal fibrosis.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Simone Giovannuzzi, Anna Nikitjuka, Bruna Rafaela Pereira Resende, Michael Smietana, Alessio Nocentini, Claudiu T. Supuran, Jean-Yves Winum
Summary: Boron-based compounds have been extensively studied in medicinal chemistry, playing a crucial role in designing small molecule drugs for various diseases. Boron is particularly valuable in developing inhibitors for metalloenzymes carbonic anhydrases, and it can modulate ligand recognition ability and selectivity. Recent advancements have led to the discovery of novel boron-based inhibitors that can inhibit carbonic anhydrases through a Lewis acid-base mechanism. Further research is needed to fully explore the potential of boron-based inhibitors and advance their clinical applications.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Xinxin Liu, Lei Chen, Ze Chen
Summary: This study developed a nanostructured photosensitizer loaded with oxygen-throttling drug and demonstrated its enhanced cytotoxicity against tumor cells under hypoxic conditions. Animal experiments showed the enhanced tumor targeting capability of the photosensitizer and its inhibitory effect on tumor growth.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Shuai Jiang, Wen-Yan Li, Zai-Feng Yuan, Qin-Shi Zhao
Summary: This study isolated two new dimeric Lycopodium alkaloids and twelve previously undescribed Lycopodium alkaloids from Lycopodiastrum casuarinoides. The structures of these compounds were determined and their inhibitory activities on the Cav3.1 channel were evaluated.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yan Yang, Dong-Xiao Yan, Rui-Xue Rong, Bing-Ye Shi, Man Zhang, Jing Liu, Jie Xin, Tao Xu, Wen-Jie Ma, Xiao-Liu Li, Ke-Rang Wang
Summary: In this study, a series of nucleolar fluorescent probes based on naphthalimide derivatives were designed and synthesized, which could achieve clear nucleolar staining in living cells. The results showed that these probes exhibited good targeting to the cell nucleolus and could bind to RNA and enhance fluorescence. This has positive implications for the diagnosis and treatment of nucleolus-related diseases.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yongxi Dong, Fang Wang, Jinlan Wen, Yongqing Mao, Shanhui Zhang, Tiemei Long, Zhangxiang Yang, Lei Li, Jiquan Zhang, Li Dong, Gang Liu, Jianwei Xu
Summary: The hybrid molecules of Scutellarein and Tertramethylpyrazine show excellent neuroprotective and antiplatelet effects in the treatment of ischemic stroke. Compound 1e is particularly effective, enhancing cell membrane permeability and inhibiting cell uptake, as well as significantly reducing cerebral infarction volume.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yu Chen, Yuanyuan Ying, Jonathan Lalsiamthara, Yuheng Zhao, Saber Imani, Xin Li, Sijing Liu, Qingjing Wang
Summary: This paper examines the role and metabolic regulation of NAD+ in bacteria, highlighting its impact on physiology and virulence. It explores enzymes associated with NAD+ metabolism as potential targets for antibacterial drugs and vaccine candidates. Additionally, it scrutinizes the medical potential of NAD+ and provides insights for its application in biomedicine.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Jon Macicior, Daniel Fernandez, Silvia Ortega-Gutierrez
Summary: Hutchinson-Gilford progeria syndrome (HGPS), also known as progeria, is a rare genetic disease that causes premature aging and significantly reduces life expectancy. Currently, there is only one approved drug for treating progeria, but its efficacy is limited. Progerin levels are believed to be the most important biomarker related to disease severity.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Fuko Hirano, Naoya Kondo, Yusuke Murata, Aya Sudani, Takashi Temma
Summary: Fluorinated alpha-methyl 3BPA derivatives showed improved water solubility, tumor targetability, and biodistribution compared to 3BPA and BPA, resulting in significantly improved tumor-to-normal tissue ratios.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Ying Shi, Jiaqin Tang, Shumeng Zhi, Ruiqi Jiang, Qing Huang, Lei Sun, Zhizhong Wang, Yanran Wu
Summary: Necroptosis is a type of cell death associated with various diseases. In this study, we identified a small molecule inhibitor, SY-1, that effectively blocks necroptosis by inhibiting the phosphorylation of RIP1/RIP3/MLKL pathway. SY-1 also showed protective effects against TNF-induced hypothermia and improved survival in mice with SIRS. These findings highlight the potential therapeutic applications of SY-1.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Andrea Bagan, Sonia Abas, Judith Pala-Pujadas, Alba Irisarri, Christian Grinan-Ferre, Merce Pallas, Itziar Muneta-Arrate, Carolina Muguruza, Luis F. Callado, Belen Perez, Elies Molins, Jose A. Morales-Garcia, Carmen Escolano
Summary: Recent studies have identified the modulation of imidazoline I-2 receptors (I-2-IR) by selective ligands as a potential strategy for treating neurodegenerative diseases. This study reports a family of bicyclic alpha-iminophosphonates that show high affinity and selectivity for I-2-IR and demonstrates their neuroprotective and anti-inflammatory effects in in vitro and in vivo models. The findings emphasize the importance of exploring structurally novel I-2-IR ligands for therapeutic strategies in neurodegeneration.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Qiuping Xiang, Tianbang Wu, Cheng Zhang, Chao Wang, Hongrui Xu, Qingqing Hu, Jiankang Hu, Guolong Luo, Xiaoxi Zhuang, Xishan Wu, Yan Zhang, Yong Xu
Summary: This study reports the discovery of a 1-(indolizin-3-yl)ethan-1-one derivative as a potent and selective CBP bromodomain inhibitor for AML drug development.
BIOORGANIC CHEMISTRY
(2024)
